Discovery of betulinic acid as a selective inhibitor of human melanoma that functions by induction of apoptosis

@article{Pisha1995DiscoveryOB,
  title={Discovery of betulinic acid as a selective inhibitor of human melanoma that functions by induction of apoptosis},
  author={Emily Pisha and Hee-byung Chai and Ik-Soo Lee and Tangai E. Chagwedera and N. R. Farnsworth and Geoffrey A. Cordell and Chris Beecher and Harry H. S. Fong and A. Douglas Kinghorn and Daniel M. Brown and Mansukh C. Wani and Monroe E. Wall and Tina J Hieken and Tapas K. Das Gupta and John M. Pezzuto},
  journal={Nature Medicine},
  year={1995},
  volume={1},
  pages={1046-1051}
}
As a result of bioassay–guided fractionation, betulinic acid, a pentacyclic triterpene, was identified as a melanoma–specific cytotoxic agent. In follow–up studies conducted with athymic mice carrying human melanomas, tumour growth was completely inhibited without toxicity. As judged by a variety of cellular responses, antitumour activity was mediated by the induction of apoptosis. Betulinic acid is inexpensive and available in abundant supply from common natural sources, notably the bark of… 

Betulinic Acid for Cancer Treatment and Prevention

  • S. Fulda
  • Biology, Chemistry
    International journal of molecular sciences
  • 2008
Compounds that exert a direct action on mitochondria present promising experimental cancer therapeutics, since they may trigger cell death under circumstances in which standard chemotherapeutics fail.

Lupane Triterpenoids—Betulin and Betulinic acid derivatives induce apoptosis in tumor cells

Investigating derivatives exerted a dose dependent antiproliferative action at micromolar concentrations toward target tumor cell lines induced apoptosis and the appearance of a typical ladder pattern in the DNA fragmentation assay.

Targeting mitochondrial apoptosis by betulinic acid in human cancers.

Development of C-20 modified betulinic acid derivatives as antitumor agents.

Betulinic acid, a natural compound with potent anticancer effects

In-vitro studies have identified this agent as potently effective against a wide variety of cancer cells, also those derived from therapy-resistant and refractory tumors, whereas it has been found to be relatively nontoxic for healthy cells.

Synthesis of betulinic acid derivatives with activity against human melanoma.

Betulinic acid: a natural product with anticancer activity.

  • S. Fulda
  • Biology, Chemistry
    Molecular nutrition & food research
  • 2009
In contrast to the potent cytotoxicity of BA against a variety of cancer types, nonmalignant cells and normal tissue remained relatively resistant to BA, indicating a therapeutic window.

Betulinic acid inhibits prostate cancer growth through inhibition of specificity protein transcription factors.

It is shown that betulinic acid decreases expression of vascular endothelial growth (VEGF) and the antiapoptotic protein survivin and acts as a novel anticancer agent through targeted degradation of Sp proteins that are highly overexpressed in tumors.
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